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Tumor Discovery A comprehensive review of bexarotene

studies revealed that bexarotene-pyrazine and bexarotene- overcame enzymatic degradation and mucociliary
2,5-dimethylpyrazine had 1.7 and 1.8 times higher clearance, enabling the drug’s delivery to the brain through
bioavailability, respectively, than commercially available the intranasal route .
[56]
bexarotene powder. The study highlights the efficacy of Aerosol formulations of bexarotene have demonstrated
the predictive model in guiding cocrystal design and
addressing absorption challenges of water-insoluble significant potential in restraining major subtypes of lung
drugs . The details of various studies have been tabulated cancer by inhibiting cell proliferation and promoting
[61]
in Table 2. apoptosis. This approach holds promise for preventing lung
cancer in high-risk populations, particularly smokers .
[57]
7.1. Amalgamation of nanomaterials with Furthermore, the development of bexarotene-loaded
bexarotene mesoporous silica frameworks has improved the drug’s
Various nanocarrier-based formulations have been solubility and bioavailability, making it suitable for topical
[59]
developed to enhance the effectiveness of bexarotene administration . In addition, lipid-based solutions and
in treating different disorders. These nanomaterials can suspensions of bexarotene have showcased improved oral
[58]
boost the drug’s efficacy by overcoming its drawbacks. bioavailability by ensuring liver microsomal stability . In
In a study, the bexarotene-loaded liposomal gel effectively another study, nanocrystals of bexarotene have exhibited
addressed the challenges of low solubility and permeability, enhanced cytotoxicity, arresting the cell cycle, and
providing an efficient treatment option for psoriasis . inducing programmed cell death. These properties make
[55]
Moreover, PEGylated PCL bexarotene nanoparticles them valuable in the treatment of lung cancer [1,6,25] .

Table 2. Compilation of formulation‑related studies
No. Formulation Objective Outcome References
1. Liposomal gel To enhance penetration and The prepared formulation improved anti-psoriatic activity [55]
therapeutic efficacy of bexarotene. and enhanced permeation by 1.8 folds in contrast to plain
bexarotene gel.
2. PEGylated To avoid rapid nasal mucociliary PEGylation reduced interactions with the mucus, showing [56]
polycaprolactone clearance, low epithelial proficient drug delivery to the brain after intranasal
nanoparticles permeation, and local enzymatic administration. The AUC brain values increased by 2 and 3 folds
degradation of bexarotene compared to non-PEGylated nanoparticles and drug dispersion,
nanoparticles. respectively.
3. Aerosols The activity of bexarotene against The aerosolized formulation showed a chemoprotective effect [57]
lung cancer. when tested against lung squamous cell carcinoma and lung
adenocarcinoma by inhibiting 68% cell proliferation and
increasing the degree of apoptosis by 4.4 folds.
4. Lipid solution and lipid Enhancement of oral The oral bioavailability was enhanced by lipid solution and lipid [58]
suspension bioavailability of bexarotene. suspension and was found to be 31.5±13.4% and 31.4±5.2%,
respectively.
5. Mesoporous silica systems To achieve the prolonged release Bexarotene-loaded mesoporous silica showed a prolonged release [59]
for topical administration and enhance the bioavailability. for 12 h with a release of 50% and hence demonstrated efficient
bexarotene delivery.
6. Nanocrystals To evaluate the antitumor activity The nanocrystals enhanced the in vitro cytotoxicity of A549 cells [25]
of bexarotene nanocrystals. with an inhibition rate of 90.26% compared to bexarotene alone
which showed an inhibition rate of 81.17%.
7. Nanocrystals for oral and Improvement of bioavailability of Nanocrystals depicted high bioavailability as AU Coral , and AUC [6]
iv
parenteral administration bexarotene. was found to be 34.83±13.61 and 40.67±2.58, respectively, in
contrast to bexarotene solution, which showed AUCoral and
AUCiv as 18.76±1.49 and 38.80±3.17, respectively.
8. Folate-chitosan Improvement of dissolution and A significant elevation in AUC 0–A74F ∞ (about 3 folds) and C max [1]
nanocrystals GIT absorption of bexarotene. (approximately 1.5 folds) resulted in enhanced drug solubility.
9. Solid dispersion Improvement of dissolution. The prepared amorphous solid dispersion with modified locust [60]
bean gum shows enhanced solubility 18 times in contrast to plain
bexarotene.
10. Cocrystals Improvement of bioavailability of Cocrystals displayed improved solubility, dissolution, and higher [61]
bexarotene. bioavailability compared to the original bexarotene powder.

Volume 2 Issue 2 (2023) 8 https://doi.org/10.36922/td.0436